青藤碱在Beagle犬体内的药动学和绝对生物利用度研究

Study on pharmacokinetics and absolute bioavailability of sinomenine in beagle dogs

目的:研究青藤碱在Beagle犬体内药动学和口服绝对生物利用度。方法:采用双周期自身交叉设计,在10只Beagle犬中研究单次口服或静脉注射青藤碱10mg·kg-1的药动学参数和绝对生物利用度,用高效液相色谱法测定血药浓度,利用3p97软件计算药动学参数。结果:口服青藤碱后犬体内药-时曲线呈一室模型,主要药动学参数Tmax(82.5±13.9)min,Cmax(0.15±0.027)mg·L-1,t1/2(87.6±28.3)min,AUC0～T(28.43±3.48)mg·min·L-1,静注青藤碱后犬体内药-时曲线呈二室模型,主要药动学参数t1/2β(106.7±120.2)min,AUC0～T(93.32±82.08)mg·min·L-1,青藤碱的口服绝对生物利用度为(30.46±4.24)%。结论:青藤碱口服绝对生物利用度较低,且在犬体内消除较快。

Objective:To study pharmacokinetic parameters and absolute bioavailability for oral use of sinomenine tablet in beagle dogs.Method:Applying to double cycle self crossover design,a single oral or intra-venous dose of 10 mg·kg-1 sinomenine was given to 10 beagle dogs.Drug concentrations in plasma were determined by HPLC.The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic program.Result:The concentration-time curves of oral administration fitted to one compartment model in the beagle dogs.Th...